4WSQ
| Crystal Structure of Adaptor Protein 2 Associated Kinase (AAK1) in complex with small molecule inhibitor | Descriptor: | 1,2-ETHANEDIOL, AP2-associated protein kinase 1, K-252A, ... | Authors: | Sorrell, F.J, Elkins, J.M, Krojer, T, Williams, E, Abdul, K, Gileadi, O, von Delft, F, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Knapp, S, Structural Genomics Consortium (SGC) | Deposit date: | 2014-10-28 | Release date: | 2014-11-05 | Last modified: | 2024-01-10 | Method: | X-RAY DIFFRACTION (1.95 Å) | Cite: | Family-wide Structural Analysis of Human Numb-Associated Protein Kinases. Structure, 24, 2016
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4WSY
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4WT6
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4X2K
| Selection of fragments for kinase inhibitor design: decoration is key | Descriptor: | 4-[(3-aminophenyl)amino]pyrido[2,3-d]pyrimidin-5(6H)-one, SULFATE ION, TGF-beta receptor type-1 | Authors: | Czodrowski, P, Hoelzemann, G, Barnickel, G, Greiner, H, Musil, D. | Deposit date: | 2014-11-26 | Release date: | 2014-12-24 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (1.69 Å) | Cite: | Selection of fragments for kinase inhibitor design: decoration is key. J.Med.Chem., 58, 2015
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4X7J
| Co-crystal Structure of PERK with 2-amino-N-[4-methoxy-3-(trifluoromethyl)phenyl]-4-methyl-3-[2-(methylamino)quinazolin-6-yl]benzamide inhibitor | Descriptor: | 2-amino-N-[4-methoxy-3-(trifluoromethyl)phenyl]-4-methyl-3-[2-(methylamino)quinazolin-6-yl]benzamide, Eukaryotic translation initiation factor 2-alpha kinase 3,Eukaryotic translation initiation factor 2-alpha kinase 3, L(+)-TARTARIC ACID | Authors: | Shaffer, P.L, Long, A.M, Chen, H. | Deposit date: | 2014-12-09 | Release date: | 2015-01-28 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Discovery of 1H-Pyrazol-3(2H)-ones as Potent and Selective Inhibitors of Protein Kinase R-like Endoplasmic Reticulum Kinase (PERK). J.Med.Chem., 58, 2015
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4WNO
| Structure of ULK1 bound to an inhibitor | Descriptor: | N~2~-(4-aminophenyl)-N~4~-(5-cyclopropyl-1H-pyrazol-3-yl)quinazoline-2,4-diamine, Serine/threonine-protein kinase ULK1 | Authors: | Lazarus, M.B, Novotny, C.J, Shokat, K.M. | Deposit date: | 2014-10-14 | Release date: | 2015-01-14 | Last modified: | 2023-09-27 | Method: | X-RAY DIFFRACTION (1.56 Å) | Cite: | Structure of the Human Autophagy Initiating Kinase ULK1 in Complex with Potent Inhibitors. Acs Chem.Biol., 10, 2015
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4WRS
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4WUA
| Crystal structure of human SRPK1 complexed to an inhibitor SRPIN340 | Descriptor: | CITRIC ACID, N-[2-(1-piperidinyl)-5-(trifluoromethyl)phenyl]-4-pyridinecarboxamide, SRSF protein kinase 1, ... | Authors: | Hoshina, M, Ikura, T, Hosoya, T, Hagiwara, M, Ito, N. | Deposit date: | 2014-10-31 | Release date: | 2015-09-16 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Identification of a Dual Inhibitor of SRPK1 and CK2 That Attenuates Pathological Angiogenesis of Macular Degeneration in Mice Mol.Pharmacol., 88, 2015
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1KV1
| p38 MAP Kinase in Complex with Inhibitor 1 | Descriptor: | 1-(5-TERT-BUTYL-2-METHYL-2H-PYRAZOL-3-YL)-3-(4-CHLORO-PHENYL)-UREA, p38 MAP kinase | Authors: | Pargellis, C, Tong, L, Churchill, L, Cirillo, P.F, Gilmore, T, Graham, A.G, Grob, P.M, Hickey, E.R, Moss, N, Pav, S, Regan, J. | Deposit date: | 2002-01-23 | Release date: | 2002-03-27 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2.5 Å) | Cite: | Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat.Struct.Biol., 9, 2002
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1KV2
| Human p38 MAP Kinase in Complex with BIRB 796 | Descriptor: | 1-(5-TERT-BUTYL-2-P-TOLYL-2H-PYRAZOL-3-YL)-3-[4-(2-MORPHOLIN-4-YL-ETHOXY)-NAPHTHALEN-1-YL]-UREA, p38 MAP kinase | Authors: | Pargellis, C, Tong, L, Churchill, L, Cirillo, P.F, Gilmore, T, Graham, A.G, Grob, P.M, Hickey, E.R, Moss, N, Pav, S, Regan, J. | Deposit date: | 2002-01-23 | Release date: | 2002-03-27 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat.Struct.Biol., 9, 2002
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1M2R
| Crystal structure of 5,8-di-amino-1,4-di-hydroxy-anthraquinone/CK2 kinase complex | Descriptor: | 5,8-DI-AMINO-1,4-DIHYDROXY-ANTHRAQUINONE, CASEIN kinase II, alpha chain | Authors: | De Moliner, E, Moro, S, Sarno, S, Zagotto, G, Zanotti, G, Pinna, L.A, Battistutta, R. | Deposit date: | 2002-06-25 | Release date: | 2003-06-17 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (1.7 Å) | Cite: | Inhibition of protein kinase CK2 by anthraquinone-related compounds. A
structural insight J.Biol.Chem., 278, 2003
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1M2P
| Crystal structure of 1,8-di-hydroxy-4-nitro-anthraquinone/CK2 kinase complex | Descriptor: | 1,8-DI-HYDROXY-4-NITRO-ANTHRAQUINONE, Casein kinase II, alpha chain | Authors: | De Moliner, E, Moro, S, Sarno, S, Zagotto, G, Zanotti, G, Pinna, L.A, Battistutta, R. | Deposit date: | 2002-06-25 | Release date: | 2003-06-17 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Inhibition of protein kinase CK2 by anthraquinone-related compounds. A
structural insight J.Biol.Chem., 278, 2003
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1MUO
| CRYSTAL STRUCTURE OF AURORA-2, AN ONCOGENIC SERINE-THREONINE KINASE | Descriptor: | ADENOSINE, Aurora-related kinase 1 | Authors: | Cheetham, G.M.T, Knegtel, R.M.A, Coll, J.T, Renwick, S.B, Swenson, L, Weber, P, Lippke, J.A, Austen, D.A. | Deposit date: | 2002-09-24 | Release date: | 2003-04-15 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2.9 Å) | Cite: | Crystal Structure of Aurora-2, an Oncogenic Serine/Threonine Kinase J.Biol.Chem., 277, 2002
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1MRU
| Intracellular Ser/Thr protein kinase domain of Mycobacterium tuberculosis PknB. | Descriptor: | MAGNESIUM ION, PHOSPHOTHIOPHOSPHORIC ACID-ADENYLATE ESTER, Probable serine/threonine-protein kinase pknB | Authors: | Young, T.A, Delagoutte, B, Endrizzi, J.A, Alber, T, TB Structural Genomics Consortium (TBSGC) | Deposit date: | 2002-09-18 | Release date: | 2003-02-11 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (3 Å) | Cite: | Structure of Mycobacterium tuberculosis PknB supports a universal activation mechanism for Ser/Thr protein kinases. Nat.Struct.Biol., 10, 2003
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1LEZ
| CRYSTAL STRUCTURE OF MAP KINASE P38 COMPLEXED TO THE DOCKING SITE ON ITS ACTIVATOR MKK3B | Descriptor: | MAP kinase kinase 3b, MITOGEN-ACTIVATED PROTEIN KINASE 14 | Authors: | Chang, C.-I, Xu, B.-E, Akella, R, Cobb, M.H, Goldsmith, E.J. | Deposit date: | 2002-04-10 | Release date: | 2002-07-10 | Last modified: | 2021-10-27 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Crystal structures of MAP kinase p38 complexed to the docking sites on its nuclear substrate MEF2A and activator MKK3b. Mol.Cell, 9, 2002
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1LPU
| Low Temperature Crystal Structure of the Apo-form of the catalytic subunit of protein kinase CK2 from Zea mays | Descriptor: | BENZAMIDINE, Protein kinase CK2 | Authors: | Niefind, K, Puetter, M, Guerra, B, Issinger, O.-G, Schomburg, D. | Deposit date: | 2002-05-08 | Release date: | 2002-05-29 | Last modified: | 2023-10-25 | Method: | X-RAY DIFFRACTION (1.86 Å) | Cite: | Inclining the purine base binding plane in protein kinase CK2 by exchanging the flanking side-chains generates a preference for ATP as a cosubstrate. J.Mol.Biol., 347, 2005
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1LEW
| CRYSTAL STRUCTURE OF MAP KINASE P38 COMPLEXED TO THE DOCKING SITE ON ITS NUCLEAR SUBSTRATE MEF2A | Descriptor: | Mitogen-activated protein kinase 14, Myocyte-specific enhancer factor 2A | Authors: | Chang, C.-I, Xu, B.-E, Akella, R, Cobb, M.H, Goldsmith, E.J. | Deposit date: | 2002-04-10 | Release date: | 2002-07-10 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Crystal structures of MAP kinase p38 complexed to the docking sites on its nuclear substrate MEF2A and activator MKK3b. Mol.Cell, 9, 2002
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1KWP
| Crystal Structure of MAPKAP2 | Descriptor: | MAP Kinase Activated Protein Kinase 2, MERCURY (II) ION | Authors: | Meng, W, Swenson, L.L, Fitzgibbon, M.J, Hayakawa, K, ter Haar, E, Behrens, A.E, Fulghum, J.R, Lippke, J.A. | Deposit date: | 2002-01-30 | Release date: | 2002-09-18 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Structure of Mitogen-activated Protein Kinase-activated Protein (MAPKAP) Kinase 2 Suggests a Bifunctional Switch That
Couples Kinase Activation with Nuclear Export J.Biol.Chem., 277, 2002
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1NA7
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1M7Q
| Crystal structure of p38 MAP kinase in complex with a dihydroquinazolinone inhibitor | Descriptor: | 1-(2,6-DICHLOROPHENYL)-5-(2,4-DIFLUOROPHENYL)-7-PIPERAZIN-1-YL-3,4-DIHYDROQUINAZOLIN-2(1H)-ONE, Mitogen-activated protein kinase 14, SULFATE ION | Authors: | Stelmach, J.E, Liu, L, Patel, S.B, Pivnichny, J.V, Scapin, G, Singh, S, Hop, C.E.C.A, Wang, Z, Cameron, P.M, Nichols, E.A, O'Keefe, S.J, O'Neill, E.A, Schmatz, D.M, Schwartz, C.D, Thompson, C.M, Zaller, D.M, Doherty, J.B. | Deposit date: | 2002-07-22 | Release date: | 2002-12-11 | Last modified: | 2024-02-14 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase. Bioorg.Med.Chem.Lett., 13, 2003
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1L3R
| Crystal Structure of a Transition State Mimic of the Catalytic Subunit of cAMP-dependent Protein Kinase | Descriptor: | (4S)-2-METHYL-2,4-PENTANEDIOL, ADENOSINE-5'-DIPHOSPHATE, ALUMINUM FLUORIDE, ... | Authors: | Madhusudan, Akamine, P, Xuong, N.-H, Taylor, S.S. | Deposit date: | 2002-02-28 | Release date: | 2002-03-20 | Last modified: | 2023-08-16 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Crystal structure of a transition state mimic of the catalytic subunit of cAMP-dependent protein kinase. Nat.Struct.Biol., 9, 2002
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1O6Y
| Catalytic domain of PknB kinase from Mycobacterium tuberculosis | Descriptor: | MAGNESIUM ION, PHOSPHOMETHYLPHOSPHONIC ACID ADENYLATE ESTER, SERINE/THREONINE-PROTEIN KINASE PKNB | Authors: | Ortiz-Lombardia, M, Pompeo, F, Boitel, B, Alzari, P.M, TB Structural Genomics Consortium (TBSGC) | Deposit date: | 2002-10-21 | Release date: | 2003-01-30 | Last modified: | 2023-12-13 | Method: | X-RAY DIFFRACTION (2.2 Å) | Cite: | Crystal Structure of the Catalytic Domain of the Pknb Serine/Threonine Kinase from Mycobacterium Tuberculosis J.Biol.Chem., 278, 2003
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1OB3
| Structure of P. falciparum PfPK5 | Descriptor: | CELL DIVISION CONTROL PROTEIN 2 HOMOLOG | Authors: | Holton, S, Merckx, A, Burgess, D, Doerig, C, Noble, M, Endicott, J. | Deposit date: | 2003-01-24 | Release date: | 2004-01-23 | Last modified: | 2024-05-08 | Method: | X-RAY DIFFRACTION (1.9 Å) | Cite: | Structures of P. Falciparum Pfpk5 Test the Cdk Regulation Paradigm and Suggest Mechanisms of Small Molecule Inhibition Structure, 11, 2003
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1NVQ
| The Complex Structure Of Checkpoint Kinase Chk1/UCN-01 | Descriptor: | 7-HYDROXYSTAUROSPORINE, Peptide ASVSA, SULFATE ION, ... | Authors: | Zhao, B, Bower, M.J, McDevitt, P.J, Zhao, H, Davis, S.T, Johanson, K.O, Green, S.M, Concha, N.O, Zhou, B.B. | Deposit date: | 2003-02-04 | Release date: | 2003-04-08 | Last modified: | 2023-08-16 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Structural Basis for Chk1 Inhibition by UCN-01 J.Biol.Chem., 277, 2002
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1LP4
| Crystal structure of a binary complex of the catalytic subunit of protein kinase CK2 with Mg-AMPPNP | Descriptor: | MAGNESIUM ION, PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER, Protein kinase CK2 | Authors: | Niefind, K, Puetter, M, Guerra, B, Issinger, O.-G, Schomburg, D. | Deposit date: | 2002-05-07 | Release date: | 2002-05-29 | Last modified: | 2024-03-13 | Method: | X-RAY DIFFRACTION (1.86 Å) | Cite: | Inclining the purine base binding plane in protein kinase CK2 by exchanging the flanking side-chains generates a preference for ATP as a cosubstrate. J.Mol.Biol., 347, 2005
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